The present invention relates to derivatives of pyrazole for use in therapy.
Hitherto, various antihyperlipemic pharmaceutical compositions have been proposed for treatment of hyperlipemia, but, they have an important demerit of causing side effects during the long term administration to the patients. For instance, clofibrate which has hitherto been generally administered as an antihyperlipemic pharmaceutical composition causes the diseases in the bile duct system and is in danger of causing cancer, and accordingly, the clinical administration of clofibrate has been restricted. On the other hand, pharmaceutical compositions containing nicotinic acid as an active ingredient for treating hyperlipemia are rarely used because of its side effect of causing flushing or eruptions on the face and skin.
5-Methylpyrazol-3-carboxylic acid had been reported to have an activity to reduce the level of serum lipid (refer to Kupiecki, F. et al., J. pharmacol. Expt. Therap., 160 (1), 166, 1968), it was proved later that in addition to the uncertainty of the derivative's clinical effect in treatment of hyperlipemia, it showed a side effect of causing the reduction of blood sugar-level and accordingly, it was not suitable as an active ingredient in the pharmaceutical composition for treating hyperlipemia (refer to Land, P. D. et al., Arzneim. Forsch., 25 (1), 117, 1975).
The inventors of the present invention, considering the above-mentioned present situation of antilipemic agents, after synthesizing and testing various compounds, has found that the derivatives of pyrazole represented by the general formula (I) shown later have an excellent antilipemic activity in common substantially without exhibiting noticeable side effects, and has attained the present invention.
The following description is the detailed explanation of the present invention.